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A kind of emtricitabine tablet and preparation method

A technology of emtricitabine and abine tablets, applied in the field of medicine, can solve problems such as poor long-term stability, and achieve the effects of increasing stability, improving stability and good dissolution stability

Active Publication Date: 2019-11-26
ANHUI BIOCHEM BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although tablet dissolution rate of the present invention has certain improvement, long-term stability is relatively poor

Method used

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  • A kind of emtricitabine tablet and preparation method
  • A kind of emtricitabine tablet and preparation method
  • A kind of emtricitabine tablet and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032]

[0033] Preparation:

[0034] (1) First get 25g cross-linked povidone and add in the fluidized bed to form cross-linked povidone microparticles, and carry out top spray coating with emtricitabine 50% ethanol solution to obtain emtricitabine drug-loaded microparticles particles;

[0035] (2) Preparation of clathrates: β-cyclodextrin is dissolved in water to form a saturated solution, and the drug-loaded microparticles prepared in step (1) are top-sprayed and coated with a weight gain of 2%. Hisabine inclusion compound;

[0036] (3) Tablet compression: Mix the clathrate prepared in step (2) with microcrystalline cellulose and the remaining crospovidone evenly, pass through a 60-mesh sieve, cold-process dry granulation, and keep the temperature at 10°C for granulation Pass through a 18-mesh sieve, mix with magnesium stearate, and press into tablets to obtain plain tablets.

[0037] (4) Tablet coating: Colorcon coating powder is mixed with 10% plain tablet coating li...

Embodiment 2

[0039]

[0040] Preparation:

[0041] (1) Granulation: first get 25g crospovidone and add in the fluidized bed to form crospovidone microparticles, carry out top spray coating with 50% ethanol solution of emtricitabine, obtain emtricitabine Binary drug-loaded microparticles;

[0042] (2) Preparation of clathrates: β-cyclodextrin is dissolved in water to form a saturated solution, and the drug-loaded microparticles prepared in step (1) are top-sprayed and coated with a weight gain of 3%. Hisabine inclusion compound;

[0043] (3) Tablet compression: Mix the clathrate prepared in step (2) with microcrystalline cellulose and the remaining crospovidone evenly, pass through a 60-mesh sieve, cold-process dry granulation, and keep the temperature at 10°C for granulation Pass through a 18-mesh sieve, mix with talcum powder, and press into tablets to obtain plain tablets.

[0044] (4) Tablet coating: Colorcon coating powder is mixed with 10% plain tablet coating liquid with 85% et...

Embodiment 3

[0046]

[0047] Preparation:

[0048] (1) Granulation: first get 25g crospovidone and add in the fluidized bed to form crospovidone microparticles, carry out top spray coating with 50% ethanol solution of emtricitabine, obtain emtricitabine Binary drug-loaded microparticles;

[0049] (2) Preparation of clathrates: β-cyclodextrin is dissolved in water to form a saturated solution, and the drug-loaded microparticles prepared in step (1) are top-sprayed and coated with a weight gain of 4%. Hisabine inclusion compound;

[0050](3) Tablet compression: mix the clathrate prepared in step (2) with microcrystalline cellulose, lactose and the remaining crospovidone evenly, pass through a 60-mesh sieve, cold-process dry granulation, and keep the temperature at 10°C After granulation, pass through a 18-mesh sieve, mix with magnesium stearate, and press into tablets to obtain plain tablets.

[0051] (4) Tablet coating: Colorcon coating powder is mixed with 10% plain tablet coating li...

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Abstract

The present invention discloses an emtricitabine tablet and a preparation method thereof, wherein the emtricitabine tablet comprises emtricitabine, a disintegrant, a coating agent, a stabilizer and a pharmaceutically acceptable excipient. The preparation method comprises: using partial disintegrant as an inner core, coating the disintegrant with emtricitabine to form micro-particles, coating the micro-particles with beta-cyclodextrin to form an emtricitabine inclusion, adding a pharmaceutically acceptable excipient and the remaining disintegrant, and coating the tablet to prepare the emtricitabine tablet. According to the present invention, the obtained emtricitabine tablet has advantages of rapid dissolution and high stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an emtricitabine tablet and a preparation method thereof. Background technique [0002] Emtricitabine (chemical name: 5-fluoro-1-(2R,5S)-[2-hydroxymethyl-1,3-oxothiocyclic-5-yl]cytosine) is a chemically synthesized cytosine nucleoside Analogs, is a newest nucleoside reverse transcriptase inhibitors. Emtricitabine is phosphorylated in multiple steps by intracellular enzymes to form Emtricitabine 5'-triphosphate, which inhibits HIV-1 reverse transcriptase by competing for natural substrates, and at the same time penetrates into the process of viral DNA synthesis, eventually resulting in disruption of DNA strand synthesis. Emtricitabine 5'-triphosphate also has weak inhibitory effects on mammalian DNA polymerase α, β, ε and mitochondrial DNA polymerase γ. By interfering with this process, which is critical for HIV replication, it helps reduce the total amount of HIV ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/28A61K31/513A61K47/61A61K47/32A61P31/18
CPCA61K9/2086A61K9/2095A61K9/2806A61K31/513
Inventor 王志邦郭立新钟晓锋沈蔡月朱礼根夏玉明陈小峰刘安友
Owner ANHUI BIOCHEM BIO PHARMA
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